化合物 azd1390|T5175|TargetMol

價格	￥678	￥980	￥1450
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 azd1390	英文名稱:azd1390
CAS:2089288-03-7	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.38%	產(chǎn)品類別: 抑制劑
貨號: T5175

Product Introduction

Bioactivity

名稱	azd1390
描述	AZD1390 is an exceptionally potent inhibitor of ATM in cells (IC50: 0.78 nM) with >10,000-fold selectivity over closely related members of the PIKK family of enzymes.
細(xì)胞實(shí)驗	Cells were seeded in six-well plates to a density of 50 to 60% and incubated at 37°C for 24 hours. Cells were pretreated with AZD1390, the ATR inhibitor AZD6738, the Wee1 inhibitor AZD1775, the poly(adenosine diphosphate-ribose) polymerase (PARP) inhibitor olaparib, or the DNA-PK inhibitor KU-0060648 at indicated concentrations for 1 hour and subsequently irradiated at 2 Gy using the Faxitron CellRad (130-kV, 5-mA, 0.5-mm Al). In washout experiments, the cell culture medium was immediately replaced and cells were incubated with or without the compound for 1, 6, and 24 hours. In all other experiments, proteins were collected at indicated time points following irradiation. Proteins were harvested by scraping the cells in radioimmunoprecipitation assay (RIPA) lysis buffer supplemented with protease and phosphatase inhibitors. Protein content was quantified using the BCA Protein Assay Kit according to manufacturing conditions. Proteins were separated by SDS–polyacrylamide gel electrophoresis on 4 to 12% bis-tris or 3 to 8% Tris-acetate gels and transferred onto nitrocellulose membranes using the iBlot Dry Blotting System. Membranes were briefly washed with water and Tris-buffered saline (TBS) with 0.05% Tween 20 (TBST) once and incubated in blocking solution, followed by primary antibodies diluted in TBST with 5% (w/v) nonfat dry milk or 3% bovine serum albumin (BSA) overnight at 4°C with shaking. Membranes were then washed three times and incubated for 1.5 hours with horseradish peroxidase (HRP)–conjugated antibodies and/or LI-COR fluorescent antibodies CW700-800 in TBST with 5% (w/v) nonfat dry milk. Membranes were washed five times with TBST, and proteins were visualized with the Fuji or Syngene G:BOX Imaging System or Film Developer after enhanced chemiluminescence substrate addition.
動物實(shí)驗	Bioluminescence signaling of implanted 3 × 10^5 NCI-H2228-Luc cells was measured using an IVIS Xenogen imaging machine to monitor tumor growth. When the signal reached the range of 10^7 to 10^8, the mice were randomized into different treatment groups and treated orally with either vehicle or AZD1390 QD or BID + IR at 2.5 Gy daily for four consecutive days. AZD1390 or vehicle was dosed at 1 hour before IR on each dosing day. The bioluminescence signals and body weight of the mice were measured once weekly, and the raw data were recorded according to their study number and measurement date in the in vivo database. TGI from the start of treatment was assessed by comparison of the mean change in bioluminescence intensity for the control and treated groups and presented as % of TGI. The calculation of inhibition and regression was based on the geometric mean of relative tumor volume (RTV) in each group. "CG" means the geometric mean of RTV of the control group, whereas "TG" means the geometric mean of RTV of the treated group. On specific day, for each treated group, the inhibition value was calculated using the following formula: Inhibition% = (CG ? TG) * 100/(CG ? 1). CG should use the corresponding control group of the treated group during calculation. If inhibition was >100%, then regression was calculated using the following formula: Regression = 1 – TG. Statistical significance was evaluated using a one-tailed t-test. Survival benefit was measured by Kaplan-Meier plots at the end of the study.
體外活性	AZD1390對ATM自磷酸化的抑制在治療后4小時發(fā)生，3 nM在LN18 GBM細(xì)胞中產(chǎn)生了強(qiáng)烈的ATM抑制效果。在相同條件下測試的其他DDR抑制劑，即便是在相關(guān)IC50濃度下，也未對pATM水平產(chǎn)生影響。在使用AZD1390及2 Gy輻射處理24小時后，觀察到G2階段累積量呈劑量依賴性增加，這表明細(xì)胞沒有在S期停滯，而是在G2階段累積或在有絲分裂過程中遇到問題。
體內(nèi)活性	在體內(nèi)同源和患者來源的膠質(zhì)瘤模型以及原位肺腦轉(zhuǎn)移模型中，AZD1390與每日分割的IR（全腦或立體定向放射治療）聯(lián)合使用，顯著促進(jìn)了腫瘤退縮并提高了動物存活率。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 4.77 mg/mL (9.98 mM), Sonication is recommended.
關(guān)鍵字	azd1390 \| ATM/ATR \| azd-1390 \| ATM and RAD3 related \| AZD 1390 \| inhibit \| Inhibitor \| Ataxia telangiectasia mutated
相關(guān)產(chǎn)品	Schisandrin B \| Ceralasertib \| AZ31 \| Berzosertib \| KU60019 \| Elimusertib \| CP-466722 \| GJ103 sodium salt \| Ro 90-7501 \| NU6027 \| (Z)-Mirin \| Dactolisib
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌活性化合物庫 \| 已知活性化合物庫 \| 激酶抑制劑庫 \| 高選擇性抑制劑庫 \| 酪氨酸激酶分子庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字： azd1390|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計算機(jī)輔助藥物設(shè)計）研究中心、藥理實(shí)驗室、藥化合成平臺三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
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公司成立：12年
注冊資本：566.265100萬人民幣
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主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號8樓

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